EP1237872B1 - Verbindungen und zusammensetzungen zur abgabe aktiver wirkstoffe - Google Patents
Verbindungen und zusammensetzungen zur abgabe aktiver wirkstoffe Download PDFInfo
- Publication number
- EP1237872B1 EP1237872B1 EP00986516A EP00986516A EP1237872B1 EP 1237872 B1 EP1237872 B1 EP 1237872B1 EP 00986516 A EP00986516 A EP 00986516A EP 00986516 A EP00986516 A EP 00986516A EP 1237872 B1 EP1237872 B1 EP 1237872B1
- Authority
- EP
- European Patent Office
- Prior art keywords
- active agent
- insulin
- hormone
- composition
- dosage unit
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
Links
- RFMJOTBAYQUWRW-UHFFFAOYSA-N COc(cc1)cc(C(Nc2ccc(CCC(O)=O)cc2)=O)c1O Chemical compound COc(cc1)cc(C(Nc2ccc(CCC(O)=O)cc2)=O)c1O RFMJOTBAYQUWRW-UHFFFAOYSA-N 0.000 description 3
- 0 C*(C)(Cc1ccc(CCC(OC)=O)cc1)C(c1cc(OC)ccc1O*)=O Chemical compound C*(C)(Cc1ccc(CCC(OC)=O)cc1)C(c1cc(OC)ccc1O*)=O 0.000 description 1
- UAAQBTSDBCUVKX-UHFFFAOYSA-N COc1ccc(C(NC2=CCC=C(CCC(O)=O)C=C2)=O)c(O)c1 Chemical compound COc1ccc(C(NC2=CCC=C(CCC(O)=O)C=C2)=O)c(O)c1 UAAQBTSDBCUVKX-UHFFFAOYSA-N 0.000 description 1
- BSSXGPNDMNAMML-UHFFFAOYSA-N OC(CCc(cc1)ccc1NC(c1ccccc1-c(cccc1)c1C(O)=O)=O)=O Chemical compound OC(CCc(cc1)ccc1NC(c1ccccc1-c(cccc1)c1C(O)=O)=O)=O BSSXGPNDMNAMML-UHFFFAOYSA-N 0.000 description 1
- GYOIBCSGVJZQMQ-UHFFFAOYSA-N OC(CCc(cc1F)ccc1NC(c1ccccc1O)=O)=O Chemical compound OC(CCc(cc1F)ccc1NC(c1ccccc1O)=O)=O GYOIBCSGVJZQMQ-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
- C07C235/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
- C07C235/44—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
- C07C235/58—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho-position to carbon atoms of the same non-condensed six-membered aromatic ring
- C07C235/60—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho-position to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
- C07C235/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
- C07C235/44—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
- C07C235/58—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho-position to carbon atoms of the same non-condensed six-membered aromatic ring
- C07C235/64—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho-position to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
- C07C235/70—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
- C07C235/84—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
- C07C237/28—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton
- C07C237/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
Claims (29)
- Eine Zusammensetzung, enthaltend:(A) einen Wirkstoff; und(B) die Verbindung aus Anspruch 1 und Gemische davon.
- Die Zusammensetzung nach Anspruch 2, wobei der Wirkstoff aus der Gruppe ausgewählt wird bestehend aus einem biologischen Wirkstoff, einem chemischen Wirkstoff und einer Kombination davon.
- Die Zusammensetzung nach Anspruch 3, wobei der biologische Wirkstoff mindestens ein Protein, Polypeptid, Peptid, Hormon, Polysaccharid, Mucopolysaccharid, Kohlenhydrat oder Lipid enthält.
- Die Zusammensetzung nach Anspruch 3, wobei der biologische Wirkstoff aus der Gruppe ausgewählt wird bestehend aus: Wachstumshormonen, menschlichen Wachstumshormonen, rekombinanten menschlichen Wachstumshormonen (rhGH), Wachstumshormonen aus Rind, Wachstumshormonen aus Schwein, Releasinghormonen der Wachstumshormone, Releasingfaktor der Wachstumshormone, Interferone, α-Interferon, β-Interferon, γ-Interferon, Interleukin-1, Interleukin-2, Insulin, Insulin aus Schwein, Insulin aus Rind, humanem Insulin, rekombinantem humanen Insulin, Insulin-ähnlichem Wachstumsfaktor (IGF), IGF-1, Heparin, unfraktioniertem Heparin, Heparinoiden, Dermatanen, Chondroitinen, Heparin geringen Molekulargewichts, Heparin sehr geringen Molekulargewichts, Heparin ultra geringen Molekulargewichts, Calcitonin, Calcitonin aus Lachs, Calcitonin aus Aal, humanem Calcitonin; Erythropoietin (EPO), atrialem natriuretischem Faktor, Antigenen, monoklonalen Antikörpern, Somatostatin, Protease-Inhibitoren, Adrenocorticotropin, Gonadotropin-Releasinghormon, Oxytocin, Releasinghormon des luteinisierenden Hormons, follikelstimulierendem Hormon, Glucocerebrosidase, Thrombopoetin, Filgrastim, Prostaglandinen, Cyclosporin, Vasopressin, Natrium-Cromolym, Natrium-Chromoglycat, Di-Natrium-Chromoglycat, Vancomycin, Desferoxamin (DFO), parathyroidem Hormon (PTH), Fragmenten von PTH, antimikrobiellen Substanzen, antifungalen Wirkstoffen, Vitaminen; Analoga, Fragmenten, Mimetika und Polyethylenglycol (PEG)-modifizierten Derivaten dieser Verbindungen; sowie jeglichen Kombination davon.
- Die Zusammensetzung nach Anspruch 3, wobei der biologische Wirkstoff Insulin, Heparin, Calcitonin, parathyroides Hormon, Erythropoietin, Wachstumshormone oder Kombinationen davon enthält.
- Die Zusammensetzung nach Anspruch 3, wobei der biologische Wirkstoff rekombinante menschliche Wachstumshormone enthält.
- Die Zusammensetzung nach Anspruch 3, wobei der biologische Wirkstoff parathyroides Hormon enthält.
- Die Zusammensetzung nach Anspruch 3, wobei der biologische Wirkstoff Insulin enthält.
- Die Zusammensetzung nach Anspruch 3, wobei der biologische Wirkstoff Heparin enthält.
- Die Zusammensetzung nach Anspruch 3, wobei der biologische Wirkstoff Calcitonin enthält.
- Die Zusammensetzung nach Anspruch 3, wobei der biologische Wirkstoff Interferon enthält.
- Eine Zusammensetzung, enthaltend:(A) einen Wirkstoff und(B) eine Poly(aminosäure), enthaltend eine Verbindung, die eine Formel aufweist ausgewählt aus der Gruppe bestehend aus den der Verbindungen nach Anspruch 1, Salze davon und Gemische davon.
- Die Zusammensetzung nach Anspruch 13, wobei die Poly(aminosäure) ein Polypeptid ist.
- Eine Einheitsdosis-Verabreichungsform, enthaltend:(A) die Zusammensetzung nach Anspruch 2, und(B) (a) einen Hilfsstoff,(b) ein Verdünnungsmittel,(c) ein Zersetzungsmittel,(d) einen Schmierstoff,(e) einen Weichmacher,(f) einen Farbstoff(g) einen Dosierungsträger, oder(h) jegliche Kombination davon.
- Die Einheitsdosis-Verabreichungsform nach Anspruch 15, wobei der Wirkstoff aus einer Gruppe ausgewählt wird bestehend aus einem biologischen Wirkstoff, einem chemischen Wirkstoff und einer Kombination davon.
- Die Einheitsdosis-Verabreichungsform nach Anspruch 16, wobei der biologische Wirkstoff mindestens ein Protein, Polypeptid, Peptid, Hormon, Polysaccharid, Mucopolysaccharid, Kohlenydrat oder Lipid enthält.
- Die Einheitsdosis-Verabreichungsform nach Anspruch 16, wobei der biologische Wirkstoff aus einer Gruppe ausgewählt wird bestehend aus: Wachstumshormonen, humanen Wachstumshormonen (hGH), rekombinanten humanen Wachstumshormonen (rhGH), Wachstumshormonen aus Rind, Wachstumshormonen aus Schwein, Releasinghormonen der Wachstumshormone, Releasingfaktor der Wachstumshormone, Interferone, α-Interferon, β-Interferon, γ-Interferon, Interleukin-1, Interleukin-2, Insulin, Insulin aus Schwein, Insulin aus Rind, humanen Insulin, rekombinantem humanen Insulin, Insulin-ähnlichem Wachstumsfaktor, Insulin-ähnlichem Wachstumsfaktor-1, Heparin, unfraktioniertem Heparin, Heparinoiden, Dermatanen, Chondroitinen, Heparin geringen Molekulargewichts, Heparin sehr geringen Molekulargewichts, Heparin ultra geringen Molekulargewichts, Calcitonin, Calcitonin aus Lachs, Calcitonin aus Aal, humanem Calcitonin; Erythropoietin (EPO), atrialem natriuretischen Faktor, Antigenen, monoklonalen Antikörpern, Somatostatin, Protease-Inhibitoren, Adrenocorticotropin, Gonadotropin-Releasinghormon, Oxytocin, Releasinghormon des luteinisierenden Hormons, follikelstimulierendem Hormon, Glucocerebrosidase, Thrombopoetin, Filgrastim, Prostaglandinen, Cyclosporin, Vasopressin, Natrium-Cromolym, Natrium-Chromoglycat, Di-Natrium-Chromoglycat, Vancomycin, Desferoxamin, parathyroidem Hormon, Fragmenten von PTH, antimikrobiellen Substanzen, antifungalen Wirkstoffen, Vitaminen; Analoga, Fragmenten, Mimetika und Polyethylenglycol-modifizierten Derivaten dieser Verbindungen; sowie jeglichen Kombination davon.
- Die Einheitsdosis-Verabreichungsform nach Anspruch 16, wobei der biologische Wirkstoff Insulin, Heparin, Calcitonin, parathyroides Hormon, Erythropoietin, humanes Wachstumshormone oder Kombinationen davon enthält.
- Die Einheitsdosis-Verabreichungsform nach Anspruch 15, wobei der Wirkstoff rekombinantes humanes Wachstumshormon enthält.
- Die Einheitsdosis-Verabreichungsform nach Anspruch 15, wobei der Wirkstoff das parathyroide Hormon enthält.
- Die Einheitsdosis-Verabreichungsform nach Anspruch 15, wobei der Wirkstoff Insulin enthält.
- Die Einheitsdosis-Verabreichungsform nach Anspruch 15, wobei der Wirkstoff Heparin enthält.
- Die Einheitsdosis-Verabreichungsform nach Anspruch 15, wobei der Wirkstoff Calcitonin enthält.
- Die Einheitsdosis-Verabreichungsform nach Anspruch 15, wobei der Wirkstoff Interferon enthält.
- Die Einheitsdosis-Verabreichungsform nach Anspruch 15, wobei die Einheitsdosis-Verabreichungsform einen Dosierungsträger enthält, enthaltend eine Tablette, eine Kapsel, ein Pulver oder eine Flüssigkeit.
- Die Einheitsdosis-Verabreichungsform nach Anspruch 15, wobei der Dosierungsträger eine Flüssigkeit ist, ausgewählt aus der Gruppe bestehend aus Wasser, 1,2-Propandiol, Ethanol und jegliche Kombination davon.
- Die Verwendung einer Verbindung nach Anspruch 1 oder Gemischen davon und eines Wirkstoffs, ausgewählt aus einem biologischen Wirkstoff, einem chemischen Wirkstoff und einer Kombination davon, zur Herstellung einer Zusammensetzung zur oralen Verabreichung an ein Tier.
- Eine Methode zur Herstellung einer Verbindung, enthaltend Mischen von:(A) mindestens einem Wirkstoffs;(B) der Verbindung nach Anspruch 1; und(C) optional einen Dosierungsträger.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US17121399P | 1999-12-16 | 1999-12-16 | |
US171213P | 1999-12-16 | ||
PCT/US2000/034329 WO2001044199A1 (en) | 1999-12-16 | 2000-12-18 | Compounds and compositions for delivering active agents |
Publications (3)
Publication Number | Publication Date |
---|---|
EP1237872A1 EP1237872A1 (de) | 2002-09-11 |
EP1237872A4 EP1237872A4 (de) | 2005-06-15 |
EP1237872B1 true EP1237872B1 (de) | 2008-02-27 |
Family
ID=22622945
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP00986516A Expired - Lifetime EP1237872B1 (de) | 1999-12-16 | 2000-12-18 | Verbindungen und zusammensetzungen zur abgabe aktiver wirkstoffe |
Country Status (8)
Country | Link |
---|---|
US (2) | US6693208B2 (de) |
EP (1) | EP1237872B1 (de) |
JP (1) | JP4850379B2 (de) |
AT (1) | ATE387430T1 (de) |
AU (1) | AU2274201A (de) |
DE (1) | DE60038183T2 (de) |
ES (1) | ES2298168T3 (de) |
WO (1) | WO2001044199A1 (de) |
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-
2000
- 2000-12-18 US US10/168,275 patent/US6693208B2/en not_active Expired - Lifetime
- 2000-12-18 ES ES00986516T patent/ES2298168T3/es not_active Expired - Lifetime
- 2000-12-18 JP JP2001544689A patent/JP4850379B2/ja not_active Expired - Fee Related
- 2000-12-18 WO PCT/US2000/034329 patent/WO2001044199A1/en active IP Right Grant
- 2000-12-18 EP EP00986516A patent/EP1237872B1/de not_active Expired - Lifetime
- 2000-12-18 DE DE60038183T patent/DE60038183T2/de not_active Expired - Lifetime
- 2000-12-18 AU AU22742/01A patent/AU2274201A/en not_active Abandoned
- 2000-12-18 AT AT00986516T patent/ATE387430T1/de not_active IP Right Cessation
-
2003
- 2003-12-31 US US10/750,138 patent/US20050042274A1/en not_active Abandoned
Also Published As
Publication number | Publication date |
---|---|
EP1237872A4 (de) | 2005-06-15 |
ES2298168T3 (es) | 2008-05-16 |
JP4850379B2 (ja) | 2012-01-11 |
DE60038183D1 (de) | 2008-04-10 |
ATE387430T1 (de) | 2008-03-15 |
JP2003516971A (ja) | 2003-05-20 |
US20050042274A1 (en) | 2005-02-24 |
US6693208B2 (en) | 2004-02-17 |
WO2001044199A1 (en) | 2001-06-21 |
EP1237872A1 (de) | 2002-09-11 |
US20030216589A1 (en) | 2003-11-20 |
AU2274201A (en) | 2001-06-25 |
DE60038183T2 (de) | 2009-02-19 |
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